SSD114 hydrochloride 是一种新型 GABA_B 受体正变构调节剂。

SSD114 hydrochloride is a novel GABA B receptor positive allosteric modulator.

Solid

GABAB receptor

In the presence of 10 μM GABA, SSD114 hydrochloride at 25 μM significantly increases (to approximately 170% above basal levels) the [S]GTPγS stimulation induced by GABA alone. SSD114 hydrochloride, added at 15 and 30 μM, induces a leftward shift of the GABA concentration-response curve with a slight concomitant increase of maximal GABA stimulation at the highest concentration. In the presence of both 15 and 30 μM SSD114 hydrochloride, the EC50 for GABA decreases by 2 and 2.5 fold, respectively, while the maximal stimulation (Emax) is potentiated only at the concentration of 30 μM, reaching 161±5.09% over the basal value . has not independently confirmed the accuracy of these methods. They are for reference only.

The onset of loss of righting reflex (LORR) is reduced by pretreatment with SSD114 hydrochloride [F (5,30) =4.55, P<0.005]. Post hoc analysis indicates that the onset of LORR is significantly lower in mouse groups pretreated with doses of SSD114 hydrochloride equal to or higher than 10 mg/kg than in vehicle-treated mice. The duration of LORR is increased by pretreatment with SSD114 hydrochloride [F (5,30) =4.81, P<0.005]. Post hoc analysis indicates that the duration of LORR is significantly longer in mouse groups pretreated with 10 and 100 mg/kg SSD114 hydrochloride than in vehicle-treated mice. has not independently confirmed the accuracy of these methods. They are for reference only.

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4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Porcu A, et al. In vitro and in vivo pharmacological characterization of SSD114, a novel GABAB positive allosteric modulator. Eur J Pharmacol. 2016 Nov 15;791:115-123.

In Vitro: DMSO : 130 mg/mL (335.20 mM; Need ultrasonic)H₂O : 2 mg/mL (5.16 mM; ultrasonic and warming and heat to 60°C)配制储备液